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Assay Detail

CHEMBL954231

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Agonist activity at rat 5HT2A receptor expressed in mouse NIH3T3 cells assessed as stimulation of inositol phosphate accumulation
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type NIH3T3
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 2A (CHEMBL322)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

'Hybrid' benzofuran-benzopyran congeners as rigid analogs of hallucinogenic phenethylamines.
Schultz DM, Prescher JA, Kidd S, Marona-Lewicka D, Nichols DE, Monte A.
Bioorg Med Chem (2008) 16 : 6242 -6251
PubMed 18467103 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 7.37 8.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL482703 1 8.03
CHEMBL520449 1 7.89
CHEMBL101008 1 7.89
CHEMBL519145 1 7.72
CHEMBL6607 BROLAMFETAMINE 2.0 1 7.66
CHEMBL520133 1 7.11
CHEMBL482704 1 6.84
CHEMBL482675 1 6.62
CHEMBL482702 1 6.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL482703 EC50 = 9.4 nM 8.03
CHEMBL520449 EC50 = 13.0 nM 7.89
CHEMBL101008 EC50 = 13.0 nM 7.89
CHEMBL519145 EC50 = 19.0 nM 7.72
CHEMBL6607 BROLAMFETAMINE EC50 = 22.0 nM 7.66
CHEMBL520133 EC50 = 78.0 nM 7.11
CHEMBL482704 EC50 = 146.0 nM 6.84
CHEMBL482675 EC50 = 241.0 nM 6.62
CHEMBL482702 EC50 = 258.0 nM 6.59